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Gastrointestinal neurotensin receptors: contribution of the aromatic hydroxyl group in position 11 to peptide potency
Author(s) -
Donoso M. Verónica,
HuidobroToro J. Pablo,
Pierre Serge
Publication year - 1986
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1986.tb10189.x
Subject(s) - neurotensin , neurotensin receptor , pharmacophore , potency , peptide , chemistry , receptor , gastric fundus , structure–activity relationship , pharmacology , in vitro , neuropeptide , stereochemistry , biochemistry , medicine , biology , stomach
Neurotensin structural analogues on tyrosine 11 were tested in vitro to determine their ability to contract the fundus or relax the intestine. The rank order of potency was: neurotensin > [Phe 11 ]‐neurotensin > [D‐Tyr 11 ]‐neurotensin > [D‐Phe 11 ]‐neurotensin. All peptides behaved as full agonists. It is concluded that tyrosine 11 is part of the neurotensin pharmacophore; the hydroxyl group increases the affinity not the intrinsic activity of the peptide at the receptor.